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詳細(xì)介紹 Vandetanib

產(chǎn)品活性：Vandetanib是有效的 VEGFR2 抑制劑，IC50 為40 nM。

研究領(lǐng)域：Protein Tyrosine Kinase/RTK | Autophagy

作用靶點：VEGFR | Autophagy

In Vitro: Vandetanib inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Vandetanib is not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM, while almost has no activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib inhibits VEGF-, EGF- and bFGF-stimulated HUVEC proliferation with IC50 of 60 nM, 170 nM and 800 nM, with no effect on basal endothelial cell growth. Vandetanib inhibits tumor cell growth with IC50 of 2.7 μM (A549) to 13.5 μM (Calu-6). Odanacatib is a weak inhibitor of antigen presentation, measured in a mouse B cell line (IC50=1.5 0.4 μM), compared to the Cat S inhibitor LHVS (IC50=0.001 μM) in the same assay. Odanacatib also shows weak inhibition of the processing of the MHC II invariant chain protein Iip10 in mouse splenocytes compared to LHVS (minimum inhibitory concentration 1-10 μM versus 0.01 μM, respectively). Vandetanib suppresses phosphorylation of VEGFR-2 in HUVECs and EGFR in hepatoma cells and inhibits cell proliferation.

In Vivo: Vandetanib (15 mg/kg, p.o.) has a superior anti-tumor effect than gefitinib in the H1650 xenograft model, and suppresses tumor growth with IC50 of 3.5 1.2 μM. In tumor-bearing mice, vandetanib (50 or 75 mg/kg) suppresses phosphorylation of VEGFR-2 and EGFR in tumor tissues, significantly reduces tumor vessel density, enhances tumor cell apoptosis, suppresses tumor growth, improves survival, reduces number of intrahepatic metastases, and upregulates VEGF, TGF-α, and EGF in tumor tissues.

相關(guān)產(chǎn)品：FDA-Approved Drug Library Plus | Drug Repurposing Compound Library | FDA-Approved Drug Library Mini | Kinase Inhibitor Library | CNS-Penetrant Compound Library | FDA-Approved Drug Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Drug Repurposing Compound Library Plus | Bioactive Compound Library Plus | Autophagy Compound Library | Sorafenib | Lenvatinib | Nintedanib | Regorafenib | Cabozantinib | Ponatinib | Sunitinib | Semaxinib | Bevacizumab | Apatinib | Pazopanib | Axitinib | PD173074 | Foretinib | SU 5402 | RAF265 | Linifanib | Cediranib | Lucitanib | Sitravatinib | BMS-690514 | Gandotinib | Tivozanib | Dovitinib | 5Z-7-Oxozeaenol | PF-03814735

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